期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 4, 页码 1569-1574出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.12.136
关键词
[C-11]GSK2126458; [F-18]GSK2126458; Phosphoinositide 3-kinase (PI3K); Mammalian target of rapamycin (mTOR); Positron emission tomography (PET); Cancer
资金
- Breast Cancer Research Foundation
- NSF-MRI [CHE-0619254]
GSK2126458 is a highly potent inhibitor of phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) with low picomolar to subnanomolar activity. [C-11]GSK2126458 and [F-18]GSK212 6458, new potential PET agents for imaging of PI3K and mTOR in cancer, were first designed and synthesized in 40-50% and 20-30% decay corrected radiochemical yield, and 370-740 and 37-222 GBq/lmol specific activity at end of bombardment (EOB), respectively. (C) 2012 Elsevier Ltd. All rights reserved.
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